Inhibition of beta-carbonic anhydrases from Brucella suis with C-cinnamoyl glycosides incorporating the phenol moiety

摘要

A small series of C-glycosides containing the phenol moiety was tested for the inhibition of the beta-class carbonic anhydrases (beta CAs, EC 4.2.1.1) from Brucella suis. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes. Glycosides incorporating the 3-hydroxyphenyl moiety showed the best inhibition profile, and therefore this functionality represents lead for the development of novel anti-infectives with a new mechanism of action.